1. Anticonvulsants can be classified into 7 categories based on their chemical structure: barbiturates, hydantoins, oxazolidinediones, succinimides, urea and monoacylureas, benzodiazepines, and miscellaneous agents.
2. Each class of anticonvulsants has characteristic structural features that contribute to their anticonvulsant effects. For example, barbiturates contain a barbituric acid core structure, while hydantoins contain a hydantoin core.
3. The most commonly used anticonvulsants include phenytoin, carbamazepine, valproic acid, and clon
Aminoglycosides(medicinal chemistry by p.ravisankar)Dr. Ravi Sankar
Aminoglycosides,Aminocyclitols,Source,Structures of streptomycin,Dihydrostreptomycin,A mention of other aminoglycoside antibiotics,Acid hydrolysis,Mechanism of action,SAR,Dihydrostreptomycin and its importance,therapeutic uses, toxicity.
General Anaesthesia (Medicinal Chemistry)Yogesh Tiwari
General anaesthetics are group of drugs that produces loss of consciousness, and therefore, loss of all sensations.
The absolute loss of sensation is termed as anaesthesia.
A condition in which the heart is unable to pump sufficient blood
to meet the metabolic demand of the body and also unable to receive it back because every time after a systole.
Calcium channel blockers - Medicinal chemistry for B.Pharm.Purna Nagasree K
This ppt describes about the drugs used as calcium channel blockers, their mechanism of action, metabolism and Structure activity relationship of dihydropyridines
depression ,symptoms, mechanism of depression ,classification of antidepressants , tri cyclic anti depressants and its pharmacological actions ,acute poisoning and treatment
Introduction to diuretics.
Therapeutic approaches.
Normal physiology of urine formation.
Classification of drugs .
Mechanism of action of Acetazolamide.
Mechanism of action of Thiazides.
Mechanism of action of Loop diuretics.
Mechanism of action of potassium sparing diuretics &aldosterone antagonists.
Aminoglycosides(medicinal chemistry by p.ravisankar)Dr. Ravi Sankar
Aminoglycosides,Aminocyclitols,Source,Structures of streptomycin,Dihydrostreptomycin,A mention of other aminoglycoside antibiotics,Acid hydrolysis,Mechanism of action,SAR,Dihydrostreptomycin and its importance,therapeutic uses, toxicity.
General Anaesthesia (Medicinal Chemistry)Yogesh Tiwari
General anaesthetics are group of drugs that produces loss of consciousness, and therefore, loss of all sensations.
The absolute loss of sensation is termed as anaesthesia.
A condition in which the heart is unable to pump sufficient blood
to meet the metabolic demand of the body and also unable to receive it back because every time after a systole.
Calcium channel blockers - Medicinal chemistry for B.Pharm.Purna Nagasree K
This ppt describes about the drugs used as calcium channel blockers, their mechanism of action, metabolism and Structure activity relationship of dihydropyridines
depression ,symptoms, mechanism of depression ,classification of antidepressants , tri cyclic anti depressants and its pharmacological actions ,acute poisoning and treatment
Introduction to diuretics.
Therapeutic approaches.
Normal physiology of urine formation.
Classification of drugs .
Mechanism of action of Acetazolamide.
Mechanism of action of Thiazides.
Mechanism of action of Loop diuretics.
Mechanism of action of potassium sparing diuretics &aldosterone antagonists.
Basic Presentation on Sedatives & Hypnotics that includes course objectives, course outcomes.
This file also contains Introduction, Classification, Structure Activity Relationship, Synthesis, Therapeutic uses of given topic.
Some questions are also covered in this file.
This ppt covers the classification, structures and IUPAC names, Mechanism of action and uses of individual drugs...under anticonvulsants topic..Side effects/metabolism are also given for few
This ppt covers the classification of anti psychotics with structures and IUPAC names, MOA, uses, metabolism and side effects. Dopaminergic pathways also given
Sympathomimetics or Adrenergic Agonists (Introduction, Classification, Adenor...Ahmad Naeem
Sympathomimetics or adrenergic agonists (introduction, classification, adenoreceptors, neurtransmission, direct acting, indirect acting, mixed action agonists, summary)
Drugs that partially or completely mimic the effects of transmitter substances of the sympathetic nervous system. On the basis of chemical structure we divide Sympathomimetics into
1. Catecholamine
2. Non-Catecholamine
Adrenergic drugs that activate adrenergic receptors are termed
as sympathomimetics, Some sympathomimetics directly activate
adrenergic receptors (direct-acting agonists), while others act
indirectly by enhancing release or blocking reuptake of norepinephrine (indirect-acting agonists). Adrenergic transmission is restricted to the sympathetic division of the ANS. There are three closely related endogenous catecholamine's (CAs).
1. Noradrenaline (NA): It acts as transmitter at postganglionic sympathetic sites (except sweat glands, hair follicles and some vasodilator fibers) and in certain areas of brain.
2. Adrenaline (Adr) It is secreted by adrenal medulla and may have a transmitter role in the brain.
3. Dopamine (DA) It is a major transmitter in basal ganglia, limbic system, CTZ, anterior pituitary, etc. and in a limited manner in the periphery
Mechanism of Action , Therapeutic uses and adverse effects of Adrenergic Agonists
1. Direct-acting agonists:
These drugs act directly on α or β receptors, producing effects similar to those that occur following stimulation of sympathetic nerves or release of epinephrine from the adrenal medulla.
Examples of direct-acting agonists include epinephrine,
norepinephrine, isoproterenol, and phenylephrine.
2. Indirect-acting agonists:
These agents may block the reuptake of norepinephrine or cause the release of norepinephrine from the cytoplasmic pools or vesicles of adrenergic neuron. The norepinephrine then traverses the synapse and binds to α or β receptors.
Examples of reuptake inhibitors and agents that cause norepinephrine release include cocaine and amphetamines,
respectively.
3. Mixed-action agonists:
Ephedrine and its stereoisomer, pseudoephedrine, both stimulate adrenoceptors directly and release norepinephrine
from the adrenergic neuron.
This presentation contains a brief introduction of Adrenergic and cholinergic systems and their function in our body.
And a brief description of some adrenergic and cholinergic agents along with their mechanism of action along with their respective Structures.
The all the content in this profile is completed by the teachers, students as well as other health care peoples.
thank you, all the respected peoples, for giving the information to complete this presentation.
this information is free to use by anyone.
Prix Galien International 2024 Forum ProgramLevi Shapiro
June 20, 2024, Prix Galien International and Jerusalem Ethics Forum in ROME. Detailed agenda including panels:
- ADVANCES IN CARDIOLOGY: A NEW PARADIGM IS COMING
- WOMEN’S HEALTH: FERTILITY PRESERVATION
- WHAT’S NEW IN THE TREATMENT OF INFECTIOUS,
ONCOLOGICAL AND INFLAMMATORY SKIN DISEASES?
- ARTIFICIAL INTELLIGENCE AND ETHICS
- GENE THERAPY
- BEYOND BORDERS: GLOBAL INITIATIVES FOR DEMOCRATIZING LIFE SCIENCE TECHNOLOGIES AND PROMOTING ACCESS TO HEALTHCARE
- ETHICAL CHALLENGES IN LIFE SCIENCES
- Prix Galien International Awards Ceremony
Title: Sense of Taste
Presenter: Dr. Faiza, Assistant Professor of Physiology
Qualifications:
MBBS (Best Graduate, AIMC Lahore)
FCPS Physiology
ICMT, CHPE, DHPE (STMU)
MPH (GC University, Faisalabad)
MBA (Virtual University of Pakistan)
Learning Objectives:
Describe the structure and function of taste buds.
Describe the relationship between the taste threshold and taste index of common substances.
Explain the chemical basis and signal transduction of taste perception for each type of primary taste sensation.
Recognize different abnormalities of taste perception and their causes.
Key Topics:
Significance of Taste Sensation:
Differentiation between pleasant and harmful food
Influence on behavior
Selection of food based on metabolic needs
Receptors of Taste:
Taste buds on the tongue
Influence of sense of smell, texture of food, and pain stimulation (e.g., by pepper)
Primary and Secondary Taste Sensations:
Primary taste sensations: Sweet, Sour, Salty, Bitter, Umami
Chemical basis and signal transduction mechanisms for each taste
Taste Threshold and Index:
Taste threshold values for Sweet (sucrose), Salty (NaCl), Sour (HCl), and Bitter (Quinine)
Taste index relationship: Inversely proportional to taste threshold
Taste Blindness:
Inability to taste certain substances, particularly thiourea compounds
Example: Phenylthiocarbamide
Structure and Function of Taste Buds:
Composition: Epithelial cells, Sustentacular/Supporting cells, Taste cells, Basal cells
Features: Taste pores, Taste hairs/microvilli, and Taste nerve fibers
Location of Taste Buds:
Found in papillae of the tongue (Fungiform, Circumvallate, Foliate)
Also present on the palate, tonsillar pillars, epiglottis, and proximal esophagus
Mechanism of Taste Stimulation:
Interaction of taste substances with receptors on microvilli
Signal transduction pathways for Umami, Sweet, Bitter, Sour, and Salty tastes
Taste Sensitivity and Adaptation:
Decrease in sensitivity with age
Rapid adaptation of taste sensation
Role of Saliva in Taste:
Dissolution of tastants to reach receptors
Washing away the stimulus
Taste Preferences and Aversions:
Mechanisms behind taste preference and aversion
Influence of receptors and neural pathways
Impact of Sensory Nerve Damage:
Degeneration of taste buds if the sensory nerve fiber is cut
Abnormalities of Taste Detection:
Conditions: Ageusia, Hypogeusia, Dysgeusia (parageusia)
Causes: Nerve damage, neurological disorders, infections, poor oral hygiene, adverse drug effects, deficiencies, aging, tobacco use, altered neurotransmitter levels
Neurotransmitters and Taste Threshold:
Effects of serotonin (5-HT) and norepinephrine (NE) on taste sensitivity
Supertasters:
25% of the population with heightened sensitivity to taste, especially bitterness
Increased number of fungiform papillae
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These simplified slides by Dr. Sidra Arshad present an overview of the non-respiratory functions of the respiratory tract.
Learning objectives:
1. Enlist the non-respiratory functions of the respiratory tract
2. Briefly explain how these functions are carried out
3. Discuss the significance of dead space
4. Differentiate between minute ventilation and alveolar ventilation
5. Describe the cough and sneeze reflexes
Study Resources:
1. Chapter 39, Guyton and Hall Textbook of Medical Physiology, 14th edition
2. Chapter 34, Ganong’s Review of Medical Physiology, 26th edition
3. Chapter 17, Human Physiology by Lauralee Sherwood, 9th edition
4. Non-respiratory functions of the lungs https://academic.oup.com/bjaed/article/13/3/98/278874
- Video recording of this lecture in English language: https://youtu.be/lK81BzxMqdo
- Video recording of this lecture in Arabic language: https://youtu.be/Ve4P0COk9OI
- Link to download the book free: https://nephrotube.blogspot.com/p/nephrotube-nephrology-books.html
- Link to NephroTube website: www.NephroTube.com
- Link to NephroTube social media accounts: https://nephrotube.blogspot.com/p/join-nephrotube-on-social-media.html
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Ethanol (CH3CH2OH), or beverage alcohol, is a two-carbon alcohol
that is rapidly distributed in the body and brain. Ethanol alters many
neurochemical systems and has rewarding and addictive properties. It
is the oldest recreational drug and likely contributes to more morbidity,
mortality, and public health costs than all illicit drugs combined. The
5th edition of the Diagnostic and Statistical Manual of Mental Disorders
(DSM-5) integrates alcohol abuse and alcohol dependence into a single
disorder called alcohol use disorder (AUD), with mild, moderate,
and severe subclassifications (American Psychiatric Association, 2013).
In the DSM-5, all types of substance abuse and dependence have been
combined into a single substance use disorder (SUD) on a continuum
from mild to severe. A diagnosis of AUD requires that at least two of
the 11 DSM-5 behaviors be present within a 12-month period (mild
AUD: 2–3 criteria; moderate AUD: 4–5 criteria; severe AUD: 6–11 criteria).
The four main behavioral effects of AUD are impaired control over
drinking, negative social consequences, risky use, and altered physiological
effects (tolerance, withdrawal). This chapter presents an overview
of the prevalence and harmful consequences of AUD in the U.S.,
the systemic nature of the disease, neurocircuitry and stages of AUD,
comorbidities, fetal alcohol spectrum disorders, genetic risk factors, and
pharmacotherapies for AUD.
Flu Vaccine Alert in Bangalore Karnatakaaddon Scans
As flu season approaches, health officials in Bangalore, Karnataka, are urging residents to get their flu vaccinations. The seasonal flu, while common, can lead to severe health complications, particularly for vulnerable populations such as young children, the elderly, and those with underlying health conditions.
Dr. Vidisha Kumari, a leading epidemiologist in Bangalore, emphasizes the importance of getting vaccinated. "The flu vaccine is our best defense against the influenza virus. It not only protects individuals but also helps prevent the spread of the virus in our communities," he says.
This year, the flu season is expected to coincide with a potential increase in other respiratory illnesses. The Karnataka Health Department has launched an awareness campaign highlighting the significance of flu vaccinations. They have set up multiple vaccination centers across Bangalore, making it convenient for residents to receive their shots.
To encourage widespread vaccination, the government is also collaborating with local schools, workplaces, and community centers to facilitate vaccination drives. Special attention is being given to ensuring that the vaccine is accessible to all, including marginalized communities who may have limited access to healthcare.
Residents are reminded that the flu vaccine is safe and effective. Common side effects are mild and may include soreness at the injection site, mild fever, or muscle aches. These side effects are generally short-lived and far less severe than the flu itself.
Healthcare providers are also stressing the importance of continuing COVID-19 precautions. Wearing masks, practicing good hand hygiene, and maintaining social distancing are still crucial, especially in crowded places.
Protect yourself and your loved ones by getting vaccinated. Together, we can help keep Bangalore healthy and safe this flu season. For more information on vaccination centers and schedules, residents can visit the Karnataka Health Department’s official website or follow their social media pages.
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NVBDCP.pptx Nation vector borne disease control programSapna Thakur
NVBDCP was launched in 2003-2004 . Vector-Borne Disease: Disease that results from an infection transmitted to humans and other animals by blood-feeding arthropods, such as mosquitoes, ticks, and fleas. Examples of vector-borne diseases include Dengue fever, West Nile Virus, Lyme disease, and malaria.
micro teaching on communication m.sc nursing.pdfAnurag Sharma
Microteaching is a unique model of practice teaching. It is a viable instrument for the. desired change in the teaching behavior or the behavior potential which, in specified types of real. classroom situations, tends to facilitate the achievement of specified types of objectives.
Couples presenting to the infertility clinic- Do they really have infertility...Sujoy Dasgupta
Dr Sujoy Dasgupta presented the study on "Couples presenting to the infertility clinic- Do they really have infertility? – The unexplored stories of non-consummation" in the 13th Congress of the Asia Pacific Initiative on Reproduction (ASPIRE 2024) at Manila on 24 May, 2024.
2. Classification of Anticonvulsant
The various structurally classified anticonvulsant can be
classified as:
1. Barbiturates: Phenobarbitone.
2. Hydantoins : Phenytoin sodium, Ethotoin, Mephenytoin
3. Oxazolidine diones: Trimethadiones, Paramethadone
4. Succinimides: Phensuximides, Methsuximides,
Ethosuximide.
5. Urea and Monoacylureas: Phenacemides,
Carbamazepines.
6. Benzodiazepines: Clonazepams, Diazepam
7. Miscellaneous: Primidones, Valproic acid.
3. General SAR of Anticonvulsant
Structure common to anticonvulsant drug:
R”=
Barbiturate =
Hydantoins =
N O
O
R
R'
R''
NH
O
N
NH
OO
R
R'
O
NH
N
NH
OO
R
R'
5. R & R’’ Should be hydrocarbon radical.
If Both R and R’ are lower alkyls, the
tendency is to be active against absence
seizures (petit mal) and not active against
generalized tonic-clonic (grand mal) OR
partial seizures.
If one of the hydrocarbon substituent's is an
aryl group, activity tends to be directed
towards generalized tonic-clonic and partial
seizures and not antiabsence activity.
6. 1. Barbiturate
Only penobarbital and mephobarbital shows
enough anticonvulsant selectivity.
The metabolism of Phenobarbital involves
p-hydroxylation, followed by conjugation
7. Phenobarbital
IUPAC: 5-ethyl-5-phenyl barbituric acid.
Brand Name: Luminal
Metabolized to p-hydroxy compound followed
by glucuronide conjugation.
Uses:
1. Sedative
2. Hypnotic
3. Anticonvulsant.
The anticonvulsant action is mainly due to the
Presence of a phenyl at 5th position.
7
8. 2. Hydantoins
These are structurally related to
barbiturates but lacking 6-oxo group.
Hydantoins are more effective as
antigeneralized tonic-clonic rather than
antiabsence activity.
All the clinically useful generalized tonic-
clonic compounds possess an aryl
substituents on the 5th position
Hydantoins with lower alkyl substituents
reportedly have antiabsence activity.
N
NH
R"
OO
R
R'
9. 1. Phenytoin:
• IUPAC: 5,5-diphenyl hydantoin.
• It is the prototype drug of
Hydantoin class
• It is prime example of an anticonvulsant
acting as a sodium channel blocker.
• The drug is useful against all seizures
except absence.
• Metabolism proceeds by stereospecific p-
hydroxylation of an aromatic ring followed
by conjugation.
O
HN
NH
O
phenytoin
10. 2. Ethotoin:
• Brand Name: Peganone
• IUPAC: 3-ethyl-5-phenyl-imidazolidine-2,4-
dione
• Metabolism: The N-dealky metabolite, is
the active compound, as well as
metabolized by p-hydroxylation, & then it is
conjugated.
• Used against generalized seizures, on an
adjunctive basis due to its low potency.
O
N
NH
O
H2C
H3C
H
11. 3. Mephenytoin:
• Brand Name: Mesantoin
• IUPAC: 5-ethyl-3methyl -5-phenyl-
hydantoin.
• Metabolism: N-dealkylated to 5-ethyl-5-
phenylhydantoin assumed that active agent.
• Counterpart of phenobarbital.
• Introduced as a sedative-hypnotic and
anticonvulsant as Nirvanol but withdrawn
because of toxicity.
• Activity spectrum similar to phenytoin.
O
N
NH
O
H3C
12. 3. Oxazolidinedione
Eg: Trimethadione, Paramethadione
• Replacement of the N-H group at position 1 of the
hydantoin system with oxygen atoms yield the
oxazolidine-2,4-dione.
• It is having antiabsence activity.
• Aryl substituted oxazolidinedione shown activity
against generalized tonic-clonic seizures but
toxicities may be the problem.
O
HN
O
O
13. 1. Trimethadione:
Brand Name: Tridione
IUPAC: 3,5,5-trimethyl-2,4-oxazolidine
Dione.
Uses: 1st drug introduced specially for treating
absence seizures.
Toxicities: Dermatological & hematological
limits its clinical use.
Metabolism: by N-demethylation to the
dimethadione. Is a calcium-T channel
blocker.
O
N
O
O
H3C
H3C CH3
15. 4. Succinimide
Eg: Phensuximide, Methsuximide, Ethosuximide
Is a cyclic imide with the formula C4H5NO2
Pyrrolidine-2,5-dione
N
CH2
O
O
R
R'
R''
16. 1. Phensuximide:
Brand Name: Milontin
IUPAC:
1-methyl-3-phenylpyrrolidine-2,5-dione
Uses: Used primarily against absence
seizures.
• The phenyl substituent confers some
activity against generalized tonic-clonic
and partial seizures.
Metabolism: N-demethylation to yield active
metabolite then p-hydroxylation.
N
CH2
O
O
H
H3C
17. 2. Methsuximide:
Brand Name: Celontin
• IUPAC:
1,3-dimethyl-3-phenylpyrrolidine-2,5-dione.
• Is found to be effective and potent than
phensuximide.
• Is used against absence and complex
partial seizures.
N
CH2
O
O
H3C
H3C
18. 3. Ethosuximide:
Brand Name: Zarontin
IUPAC:
3-ethyl-3-methylpyrrolidine-2,5-dione.
• It is calcium T channel blocking drug.
• Major metabolite is produced by oxidation
of ethyl group.
• Use:
Conforms very well to the general
structural pattern for antiabsence activity.
N
CH2
O
O
H3C
CH2
H
CH3
19. 5. Urea and Monoacylureas:
Eg: Phenacetamide, Carbamazepine.
Long History of producing compounds with
anticonvulsant activity.
1. Phenacemide:
IUPAC: Phenyl acetyl urea
Use:
• Possess good anticonvulsant activity.
• Less therapeutic value in petit mal, grand mal
and mixed seizures.
H2
C
O
H
N C
O
NH2
phenylacetyl urea
20. 2. Carbamazepine:
Brand Name: Tegretol
• The Two Phenyls substituted on
the urea nitrogen fit the pattern of antigeneralized
tonic activity.
• The overall shape suggest the mode of action,
sodium channel block.
• Use: Generalized tonic-clonic and partial
seizures.
• Toxicity: potential hematological toxicity.
• Metabolism: Proceeds largely through the
epoxide formed at the (Z)cis-stilbine double bond.
Then coverts to the 10s, 11s-trans-diol.
N
O NH2
21. • The epoxide is a suspect in the idiosyncratic
reactions
• thus, oxcarbazepine were developed.
22. 6. Benzodiazepine
Eg: Clonazepam, Diazepam, Chlorazepam.
Detail study regarding Chemistry and
SAR were sees in anxiolytic-sedative-hypnotic
drugs.
Animal models predict that it modestly
effective against generalized tonic-clonic and
partial seizures and very highly active against
absence seizures.
23. 1. Clonazepam
• IUPAC: 5-(2-chlorophenyl)-3-dihydro-7-nitro-2H-
1,4-benzodiazpin-2-one
• Brand Name: Klonopin
• Uses: in absence seizure
• Tolerance often developed
• Metabolism: Hydroxtlation of the 3 position,
followed by glucuronidation.
• Nitro group reduction followed by acetylation.
O
C
N
H
O2N C
Cl
N
CH2
24. 2. Diazepam
IUPAC: 7-chloro-1,3-dihydro-1-methyl
-5-phenyl-1,4-bezodiazepin-2-one.
Brand Name: Valium
Was the 1st member of the
benzodiazepin-2-one group.
• It is very nonpolar and rapidly absorb.
USES: Anxiolytics in low doses
Antiepileptics
Central muscle relaxant
METABOLISM: By N-demethylation to nordazepam which is
then covert to oxazepam then excreted by glucuronide
conjugation.
25. 7. Miscellanious agents
Eg: Primidone & Valproic acid.
1. Primidone:
IUPAC: 5-ethyldihydro5-phenyl-
4,6-(1H,5H)-pyrimidinedione
Brand Name: Mysoline.
• Also Called as 2-deoxybarbiturates.
Uses: Against all types of Seizures except
absence.
N
O
C
H2
N
CH2
H
O
H3C
H
26. 2. Valproic Acid
IUPAC: 2-propylpentoic acid
Brand name: Depakene
SAR:
1. Activity increase with increasing chain length.
2. Introduction of double bond decreases the
activity.
3. Introduction of sec. or ter. Hydroxyl group or
replacement of carboxyl by hydroxyl group has
no effect.
MOA:
Act on GABA deactivating Enzyme.
COOH
C
H2
CH2
H2
CH3C
H2
CH3C
27. Metabolism: by conjugation of the
carboxylic acid group and oxidation of the
one of the hydrocarbon chains.
USES:
Active against typical and atypical
absences seizures and absence seizures
with generalized tonic-clonic seizures.